Everolimus. Novartis

Curr Opin Investig Drugs. 2001 Sep;2(9):1220-34.

Abstract

Everolimus (RAD-001, SDZ RAD, Certican), an analog of sirolimus, is an oral immunosuppressant that inhibits growth factor-induced cell proliferation, under development by Novartis as a potential treatment for transplant rejection. Phase III trials were initiated by the end of 1998 [319337] and were ongoing in February 2001 [400448]. At the end of 2000, Novartis was hoping to file for approval of the compound in 2001 [392881], with a possible launch in mild-2002 [392881], [401979]. Completion of phase III trials in heart transplant patients is expected this year and lung and liver transplants by 2003. In 1999, American Home Products (AHP) initiated an action for infringement of the patent EP-00401747, which covers the use of sirolimus in transplantation in the UK, the Netherlands and Germany, seeking to restrain the clinical trial program for everolimus. Novartis subsequently filed a counterclaim for invalidity. In December 1999, the UK High Court of Justice ruled that everolimus infringes the British counterpart of EP-00401747 [349637]. In contrast, in April 2000, the District Court of The Hague ruled that everolimus does not infringe patent rights licensed to AHP [362823] and in July 2000, The Court of Appeal in the UK came to the same conclusion [376559]. In February 2001, the Opposition Board at the European Patent Office upheld Novartis' European patent for everolimus, which the Board held to be 'inventive' [400448]. In July 2000, Vontobel estimated sales of SFr 80 million in 2002, rising to SFr 800 million in 2004 [378871]. In February 2001, Merrill Lynch predicted sales of SFr 125 million rising to SFr 661 million in 2005 [411704].

Publication types

  • Review

MeSH terms

  • Animals
  • Clinical Trials, Phase I as Topic
  • Clinical Trials, Phase II as Topic
  • Clinical Trials, Phase III as Topic
  • Everolimus
  • Graft Rejection / prevention & control*
  • Humans
  • Immunosuppressive Agents / adverse effects
  • Immunosuppressive Agents / chemical synthesis
  • Immunosuppressive Agents / metabolism
  • Immunosuppressive Agents / pharmacology
  • Immunosuppressive Agents / therapeutic use*
  • Sirolimus / adverse effects
  • Sirolimus / analogs & derivatives
  • Sirolimus / chemical synthesis
  • Sirolimus / metabolism
  • Sirolimus / pharmacology
  • Sirolimus / therapeutic use*
  • Structure-Activity Relationship

Substances

  • Immunosuppressive Agents
  • Everolimus
  • Sirolimus